Bisnaphthalimidopropyl spermidine induces apoptosis within colon carcinoma cells

Lynda D Ralton, Charles S Bestwick, Lesley Milne, Susan Duthie, Paul Kong Thoo Lin

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)


Bisnaphthalimido compounds bisintercalate to DNA via the major groove and are potentially potent cancer therapeutics. We incorporated natural polyamines as linkers connecting the two-naphthalimido ring moieties to create a series of novel soluble cytotoxic bisnaphthalimidopropyl polyamines (BNIPPs). Here, we determined the cytotoxicity of bisnaphthalimidopropyl spermidine (BNIPSpd) towards Caco-2 and HT-29 colon adenocarcinoma cells revealing an IC50 value of 0.15 and 1.64 mu M after 48 h exposure within Caco-2 and HT-29 cells, respectively. After 4 h. >0.5 mu M BNIPSpd treatment-induced significant DNA damage. After 24 h exposure a concentration-dependent increase in active caspase-3 expression, chromatin condensation and internucleosomal DNA fragmentation identified apoptosis as the principal manifestation for the cytotoxicity within both cell lines. By 24 h exposure, there was also a significant decline in cellular spermine and spermidine levels. It is concluded that bisnaphthalimidopropyl spermidine (BNIPSpd) toxicity primarily results from apoptosis and that BNISpd has potential to be further developed as an anti-tumour agent.

Original languageEnglish
Pages (from-to)1-6
Number of pages6
JournalChemico-Biological Interactions
Issue number1
Early online date15 Oct 2008
Publication statusPublished - 15 Jan 2009


  • DNA damage
  • bisnaphthalimidopropylpolyamines
  • polyamines
  • apoptosis
  • colon cancer
  • improved seperation systems
  • oxidative DNA-damage
  • bis-naphthalimides
  • polyamine depletion
  • liquid-chromatography
  • biological-activities
  • antitumor agents
  • in-vitro
  • derivatives
  • anoikis


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